The present invention relates to ectoparasite control compositions, methods of controlling ectoparasites and uses of a composition for controlling an ectoparasite.
It is well known in the art that when ectoparasites infest a host animal, imidacloprid can be utilized in liquid compositions to control the ectoparasites. In utilizing such liquid compositions to control an ectoparasite, said liquid compositions are sometimes spread or dropped onto the surface of the host animal infested with the ectoparasite. Such liquid compositions utilizing therein imidacloprid, provide an insufficient residual effect over the ectoparasite, as said liquid compositions are utilized to control the ectoparasite over an extended time period.
It is also well known that a pesticidal control effect can be provided by 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine. EP 0 976 328 A2 describes an ectoparasite-controlling agent for animals comprising 0.1 to 20% by weight of a neonicotinoid compound and 10 to 95% by weight of a glycol or glycol monoalkyl ether.
The present invention provides ectoparasite control compositions, ectoparasite control methods and uses for controlling ectoparasite. The ectoparasite control compositions comprise a solvent and 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine, wherein said solvent contains mainly N-methyl-2-pyrrolidone. The ectoparasite control methods comprise applying to a host animal, a composition comprising a solvent and 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine, wherein said solvent contains mainly N-methyl-2-pyrrolidone.
The ectoparasite control compositions of the present invention typically utilize therein a solvent and a effective amount of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine. The solvent in the ectoparasite control compositions contain mainly N-methyl-2-pyrrolidone. The solvent is usually present in the ectoparasite control compositions in an amount of from 40 to 99.9% by weight, wherein said weight percentage is based on the total weight of the provided ectoparasite control compositions. An effective amount of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine in the ectoparasite control compositions can be an amount of from 0.1 to 30% by weight, and preferably is 1 to 30% by weight, wherein said weight percentages are based on the total amount of the provided ectoparasite control compositions.
As used herein, the phrase xe2x80x9ccontains mainly N-methyl-2-pyrrolidonexe2x80x9d means that the provided solvent contains at least 90% by weight of N-methyl-2-pyrrolidone, wherein said weight percentage of N-methyl-2-pyrrolidone is based on the total weight of the solvent utilized in the provided ectoparasite control compositions. For example, such a solvent may consist essentially of N-methyl-2-pyrrolidone. When utilizing said solvent consisting essentially of N-methyl-2-pyrrolidone, the ectoparasite control compositions can comprise the solvent in an amount of from 85 to 99.9% by weight or from 95% to 99.9% by weight, wherein said weight percentages of the solvent are based on the total weight of the provided ectoparasite control composition.
To produce the solvent, N-methyl-2-pyrrolidone may be mixed with various liquid solvents well known in the art. For example, the solvent may involve utilizing therein N-methyl-2-pyrrolidone with alcohols, propylene carboxylate, xcex3-butyrolactone, water or the like. As examples of the alcohols, there are mentioned glycols, ethyl alcohol, isopropyl alcohol, benzyl alcohol and the like. As examples of the glycols, there are mentioned propylene glycol, hexylene glycol, diethylene glycol, dipropylene glycol, tripropylene glycol, diethylene glycol monoalkyl ether, propylene glycol monoalkyl ether, dipropylene glycol monoalkyl ether, ethylene glycol monophenyl ether and the like.
As needed, the ectoparasite control compositions may additionally comprise an auxiliary. Auxiliaries that may be useful in the ectoparasite control compositions include anti-oxidants, colorants, light stabilizers, sticking agents and the like. When utilizing the auxiliaries in the ectoparasite control compositions, an auxiliary may be present in the ectoparasite control composition in an amount of from 0.0001 to 1% by weight, wherein said weight percentages are based on the total weight of the provided ectoparasite control composition.
When the solvent involves a mixture of N-methyl-2-pyrrolidone and water, a pH adjusting agent may be added to the ectoparasite control compositions, if so desired. As examples of the pH adjusting agent, for example, there can be mentioned citric acid, sodium dihydrogen citrate, sodium hydrogen citrate, potassium hydrogen phosphate, sodium dihydrogen phosphate, ammonium dihydrogen phosphate, ammonium benzoate, sodium benzoate, boric acid, tartaric acid, succinic acid, lactic acid and the like. Such pH adjusting agents are typically utilized in the ectoparasite control compositions to maintain a pH of from 5 to 7 pH. For example, the pH adjusting agent may be present in the ectoparasite control compositions in an amount of from 0.01 to 1% by weight, wherein said weight percentage of the pH adjusting agent is based on the total weight of the water in the ectoparasite control compositions.
As examples of the anti-oxidant, there are mentioned BHT, BHA and the like.
As examples of the colorant, there are mentioned food tar dyes such as food yellow 4 (tartrazine), food green 3 (fast green FCF), food blue 1 ( brilliant blue FCF) and the like.
As examples of the light stabilizers, there are mentioned benzophenone compounds, benzotriazole compounds and the like.
As examples of the sticking agent, there are mentioned cellulose derivatives, starch derivatives, polyacrylates, naturally-occurring polymers, alginic acid salts, gelatin and the like.
The ectoparasite control compositions may also comprise a pesticidal compound in addition to 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine. By utilizing such an additional pesticidal compound in the ectoparasite control composition, a more specialized control over the ectoparasite may be provided by the ectoparasite control composition. To provide such a specialized control over the ectoparasite, 0.05 to 50% by weight of the additional pesticidal compound may be added to the ectoparasite control compositions. As examples of such additional pesticidal compounds, there are mentioned pyrethroid compounds such as phenothrin, permethrin, etofenprox, resmethrin, fenpropathrin, cyphenothrin and flumethrin, organophosphorus compounds such as tetrachlorvinphos and fenthion; carbamate compounds such as propoxur, carbaryl and fenobucarb; chitin synthesis inhibitors such as lufenuron, novaluron and chlorfluazuron; juvenile hormone analogs such as pyriproxyfen, fenoxycarb and methoprene; neonicotinoid compounds such as nitenpyram and thiamethoxam; N-phenylpyrazole compounds and the like.
The ectoparasite control compositions can be produced, for example, by mixing the solvent with 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine. When also utilizing therein an auxiliary or additional pesticidal compound, the auxiliary or additional pesticidal compound may be mixed with the solvent and 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine.
The ectoparasite control compositions are typically regionally applied to the host animal, in order to treat the host animal when infested with an ectoparasite or to prevent the host animal from being infected with an ectoparasite. Exemplary forms of such regional application can involve spot-on applications, pour-on applications and the like. In the spot-on applications the ectoparasite control compositions may be spread or added drop-wise to the skin at a back area between the shoulders of the host animal. In the pour-on applications, the ectoparasite control compositions may be poured along the spine of the host animal.
The application amount to a host animal of the ectoparastie control compositions may change depending on the type of host animal or the type of ectoparasite. For example, the ectoparasite control compositions may be applied to the host animals in an amount such that 0.05 to 1000 mg of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine is applied for every 1 kg of the host animal (i.e., 0.05 to 1000 mg/kg). Alternatively, the ectoparastite control compositions may be applied to the host animal, such that 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine is applied in an amount of from 0.1 to 200 mg/kg.
When regionally applying the ectoparasite control compositions to the host animal, the host animal may already be infested with the ectoparasites or may be uninfected with ectoparasites. As examples of such host animals, there are mentioned animals host to ectoparasites, such as animals raised as farm animals or pets. Examples of such host animals include mammal animals, birds and the like. Examples of the mammalian animals include carnivora such as dogs, cats and ferrets; Artiodactyla such as cows, sheeps, goats and swines; rodents (Rodentia) such as mice, rats, hamsters and squirrels; Lagomorpha such as rabbits, primates such as monkeys and the like. Examples of the birds include Anseriformes such as ducks, doves (Columbiformes) such as pigeons, cockatoos (Psittaciformes) such as parrots and the like.
In general, the ectoparasites that can be controlled with the ectoparasite control compositions are arthropods. As examples of such arthropods, there are mentioned Diptera pests such as houseflies (Musca domestica), Musca hervei, Musca bezzi, Haematobia irritans, Simulium iwatens, Culicoides oxystoma, Tabanus chrysurus, common mosquito (Culex pipiens) and Aedes albopictus; lice pests (Anoplura) such as cattle lice (Haematopinus eurysternus) and sheep lice (Damalinia ovis); tick pests (Acarina) such as Haemaphysalis longiconis and Boophilus microplus; fleas (Siphonaptera) such as cat fleas (Ctenocephalides felis), dog fleas (Ctenocephalides canis) and oriental rat flea (Xenopsylla cheopis) and the like.
As an example of the ectoparasite control compositions, there can be mentioned an ectoparasite control composition composed of (a) 0.1 to 30% by weight of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine and (b) 40 to 99.9% by weight of the solvent containing mainly N-methyl-2-pyrrolidone, wherein said weight percentages are based on the total weight of the provided ectoparasite control compositions.
As another example of the ectoparasite control compositions, there can be mentioned an ectoparasite control composition composed of (a) 0.1 to 30% by weight of 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine, (b) 40 to 99.9% by weight of the solvent containing mainly N-methyl-2-pyrrolidone and (c) 0.05 to 50% by weight of at least one additional pesticidal compound selected from a pyrethroid compound and a juvenile hormone analog, wherein said weight percentages are based on the total weight of the provided ectoparasite control composition.